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新型喹啉类蛋白酪氨酸激酶抑制剂的合成
引用本文:史祥飞,薛阳,赵砚瑾,李庶心. 新型喹啉类蛋白酪氨酸激酶抑制剂的合成[J]. 解放军药学学报, 2011, 27(3): 189-192. DOI: 10.3969/j.issn.1008-9926.2011.03.01
作者姓名:史祥飞  薛阳  赵砚瑾  李庶心
作者单位:1. 军事医学科学院放射与辐射医学研究所,北京,100850
2. 总后勤部管理局第一门诊部,北京,100842
3. 100850,北京,军事医学科学院放射与辐射医学研究所;100048,北京,首都师范大学生命科学院
摘    要:目的 设计合成一系列新型喹啉双芳基脲类化合物作为潜在的蛋白酪氨酸激酶抑制剂.方法 以2-甲基-2苯基丙酸为原料经过9步反应,合成了12个喹啉衍生物,结构经过1H-NMR鉴定.结果 合成的12个目标化合物,均未见文献报道.结论 该合成方法简单易行,可作为一系列喹啉类蛋白酪氨酸激酶抑制剂的合成通法.

关 键 词:肿瘤  蛋白酪氨酸激酶  蛋白酪氨酸激酶抑制剂  喹啉衍生物  合成

Design and Synthesis of Quinoline Derivatives as Protein Tyrosine Kinase Inhibitors
SHI Xiang-fei,XUE Yang,ZHAO Yan-jin,LI Shu-xin. Design and Synthesis of Quinoline Derivatives as Protein Tyrosine Kinase Inhibitors[J]. Pharmaceutical Journal of Chinese People's Liberation Army, 2011, 27(3): 189-192. DOI: 10.3969/j.issn.1008-9926.2011.03.01
Authors:SHI Xiang-fei  XUE Yang  ZHAO Yan-jin  LI Shu-xin
Affiliation:①③①Beijing Institute of Radiation Medicine,Beijing100850,China;②First Clinic of General Logistic Department,Beijing100842,China;③College of Life Sciences,Capital Normal University,Beijing100048,China
Abstract:Objective To synthesize novel quinoline derivatives as antitumor drug candidates.Methods 12 derivatives of quinoline were synthesized in nine steps from 2-methyl-2-phenylpropanoic acid.Their structures were identified by 1H-NMR.Results Twelve novel compounds were synthesized.Conclusion This method can be a general method to synthesize a series of novel quinoline derivatives as protein tyrosine kinase inhibitors.
Keywords:cancer  protein tyrosine kinase  protein tyrosine kinase inhibitors  quinoline derivatives  synthesis  
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